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Antiprotozoal and anthelmintics
15-04-2018
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Antiprotozoal Drugs
• Metronidazole
• Tinidazole
Penetrate protozoal and bacterial cells but not mammalian cells.
Work as an electron sink, so, reduced at 5-nitro group.
Nitroreductase is only found in anaerobic organisms.
The reduced molecule disrupts replication and transcription and
inhibits DNA repair.
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Metronidazole Spectrum of Activity:
E. histolytica
G. lamblia
T. vaginalis
Blastocystis hominis
B. coli
Dracunculus medinensis
Also anaerobic G+ve and G-ve bacteria
Resistance is rare.
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Metronidazole Kinetics: Good absorption and distribution,
t½ 8h.
Metabolized by oxidation and glucocuronide formation.
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Metronidazole Clinical Uses:
• All forms of amebiasis, except for the cyst passers (Diloxanide
Furoate, Paromomycin or diiodohydroxyquin).
• Giardiasis.
• Trichomoniasis.
• Anaerobic bacterial infection( in dentistry).
• D. medinensis (guinea worm).
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Adverse Reactions:
Nausea, headache, dry mouth and metallic taste.
Urine discoloration.
Vertigo, unsteadiness, ataxia, parasthesia,
neuropathy, encephalopathy.
Neutropenia.
Disulfiram-like reaction.
• Tinidazole is better tolerated.
Metronidazole
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Diloxanide Furoate
• Effective luminal amebicide.
• Mechanism unknown.
• Drug of choice for asymptomatic cyst passers.
• Flatulence, nausea, cramps, rashes.
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Antibiotics
Erythromycin
Tetracycline
Alter bacterial flora and prevent secondary infection.
Paromomycin:
• Aminoglycoside.
• Direct action on ameba in the lumen.
• Anthelminthic and for visceral leishmaniasis.
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Anthelmintic Drugs
Albendazole: Broad spectrum, which inhibits microtubule synthesis.
• Hydatid disease.
• Cysticercosis: usually given with corticosteroids to decrease
inflammation caused by dying organisms.
• Pinworm.
• Hookworm.
• Ascariasis.
• Trichuriasis.
• Strongyloidiasis.
• Others
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Anthelmintic Drugs
Bithionol:
•Drug of choice for Fascioliasis.
•Alternative drug for pulmonary paragonimiasis.
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Anthelmintic Drugs
Diethylcarbamazepine Citrate:
• Drug of choice for the treatment and prophylaxis of:
Filariasis: W. bancrofti, Brugia malayi, B.timori.
Loiasis: Loa loa.
Tropical eosinophilia: Monsonella streptoceca.
Immobilizes micrifilaria and alters their surface structure, displacing them from tissues and making them susceptible to destruction by host defense mechanisms.
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Anthelmintic Drugs
Doxycycline:
• W. bancrofti.
• Onchocerciasis.
• Works indirectly, by killing Wolbachia, an intracellular
bacterial symbiont of filarial parasites.
• Used for treatment and mass chemotherapy
campaigns.
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Anthelmintic Drugs
Ivermectin:
Strongyloidosis:
Paralyzes nematodes and arthropods by intensifying
GABA mediated transmission of signals in peripheral
nerves.
• Onchocerciasis:
Blocks the release of microfilaria for some months after
therapy.
Also effective in controlling scabies, lice, and
cutaneous larva migrans.
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Ivermectin:
Mazotti Reaction:
Occurs in 5-30% of patients, usually mild.
Due to killing of microfilaria.
Fever, headache, dizziness, somnolence,
weakness, rash, pruritus, diarrhea, joint and
muscle pains, hypotension, tachycardia
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Anthelmintic Drugs
Mebendazole:
• Wide spectrum.
• Inhibits microtubule synthesis.
• Ascariasis.
• Trichuriasis.
• Hookworm.
• Pinworm.
• Tablets chewed before swallowing.
• Safe drug.
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Anthelmintic Drugs
Metrifonate: • Schistosoma haematobium.
• Not for S. mansoni or S. japonicum.
• Organophosphate, inhibits cholinesterase, and thus paralyzes
the worm, resulting in their shift from the bladder venous
plexus to the small arterioles of the lung, where they are
trapped, encased by the immune system and die.
• Treatment.
• Mass treatment programs.
• Prophylaxis.
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Anthelmintic Drugs
Niclosamide:
Second-line drug for most tapeworm infections.
• Kills adult worms, but not the ova.
• Works by inhibition of oxidative phosphorylation.
• 2 gm single dose on an empty stomach, chewed
and swallowed.
Purgative needed.
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Anthelmintic Drugs
Oxamniquine:
• Alternative to praziquantel for the treatment of S.
mansoni , not for the others.
• Worms are detached from terminal venules in the
mesentery and transit to the liver, where they die.
• Also for massive treatment.
• Safe drug.
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Anthelmintic Drugs
Piperazine:
• Ascariasis.
• Causes paralysis by blocking acetylcholine, worms
expelled by normal peristalsis.
70 mg/day for 2-8 days.
Or, repeat after 2 weeks.
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Anthelmintic Drugs
Praziquantel:
• Schistosomes, all species, drug of choice.
• Trematodes: Clonorchiasis, Opisthorchiasis and Paragonimiasis
• Cestodes including cysticercosis.
• Increases permeability of the worm to calcium, resulting in paralysis, dislodgment and death.
• Mild and transient adverse effects, except for neurocysticercosis.
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Anthelmintic Drugs
Pyrantel Pamoate: Broad spectrum:
Pinworm.
Ascaris.
Trichostrongylus orientalis.
Hookworms.
Effective within the intestinal tract, not in the tissues or against the ova.
Works as a neuromuscular blocker.
11 mg/kg, single dose
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Pancreatic Enzymes
These medications contain digestive enzymes to
help break down and digest fats, starch, and
proteins in food.
Extracts of hog pancreas.
Used in conditions where the pancreas cannot
make or does not release enough digestive
enzymes into the small intestines to digest the food
(e.g., chronic pancreatitis, cystic fibrosis, cancer of
the pancreas, post-pancreatectomy, post-
gastrointestinal bypass surgery).
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Pancrelipase
• Available in sizes with different amounts of lipase,
amylase and protease.
• Dose should be adjusted according to age, weight,
degree of pancreatic insufficiency, and the amount
of dietary fat intake.
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Pancrelipase
• Taken with plenty of fluids.
• Used regularly to get the most benefit from it.
• Taken with every meal or snack.
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Pancrelipase
• Side Effects:
• Diarrhea, constipation, headache, abdominal
pain/cramps/bloating, gas, dizziness, cough,
nausea, or vomiting.
• May cause mucositis if not swallowed quickly.
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Bile Acid therapy for Gallstones
• Ursodiol:
• Naturally occurring bile acid, from bears.
• Absorbed in the g.i.t. and conjugated in the liver with
glycine or taurine, and excreted in the bile.
• Blocks hepatic cholesterol synthesis and thereby
decreases secretion of cholesterol by the liver and
the amount of cholesterol in bile
• Also, stabilizes hepatocyte canalicular membranes.
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Bile Acid therapy for Gallstones
• Clinical Uses:
• To dissolve small cholesterol gallstones in patients
who refuse cholecystectomy or who are poor
surgical candidtes.
• Prevention of gallstones in obese patients.
• Early stage biliary cirrhosis.
• Free of side effects.